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DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO
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Miglustat- to treat Type 1 Gaucher disease (GD1)
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| Miglustat | |
| (2R,3R,4R,5S)-1-butyl-2-(hydroxymethyl)piperidine-3,4,5-triol |
PATENT-US 5,525,616, US 5,472,969 TO Actelion Pharms Ltd
Miglustat is a drug developed by Actelion and is used primarily to treat Type 1 Gaucher disease (GD1). It is marketed under the trade name Zavesca. Miglustat (OGT 918, N-butyl-deoxynojirimycin) is an imino sugar (molecular weight: 219 daltons), a synthetic analogue of D-glucose and a white to off-white crystalline solid that has a bitter taste The primary pharmacological activity of miglustat is inhibition of the enzyme glucosylceramide synthase, catalyzing the first step in the biosynthesis of glycosphingolipids (GSL), i.e., the formation of glucosylceramide (GlcCer). Reduced formation of GlcCer will lead to decreased biosynthesis of more complex GSL. This therapeutic principle, called substrate reduction therapy (SRT), may be useful in disorders of intracellular (predominantly lysosomal) accumulation of GSL either due to their deficient breakdown or intracellular transport/trafficking. Miglustat exhibits a large volume of distribution and has the capacity to access deep organs such as the brain, bone and lung.
Miglustat is a synthetic derivative of a family of polyhydroxylated alkaloids or amino sugar extracted from plants and microorganisms. Its synthesis starts from D-glucose sugar in plants. The sugar then aminated and oxidized to amino fructose sugar, which then can form a cyclic aminohemiacetal called nojirimycin. Then the dehydration and reduction takes place successively before the formation of deoxynojirimycin, which is a precursor of miglustat. Since it is a synthetic derivative drug, alkylation ofdeoxynojirimycin can be synthesized in the laboratory with 1-butyl halide via amine alkylation.
Miglustat
CAS : 72599-27-0
(2R,3R,4R,5S)-1-Butyl-2-(hydroxymethyl)-3,4,5-piperidinetriol
Additional Names: N-butyldeoxynojirimycin; N-butylmoranoline
Manufacturers’ Codes: OGT-918; SC-48334
Trademarks: Zavesca (Actelion)
Molecular Formula: C10H21NO4
Molecular Weight: 219.28
C 54.77%, H 9.65%, N 6.39%, O 29.19%
Literature Ref: Amino sugar; inhibitor of glucosyltransferase, an enzyme involved in the biosynthesis of glycosphingolipids.
Prepn: B. Junge et al., DE 2758025; see also, eidem, US 4639436 (1979, 1987 both to Bayer).
Improved synthesis: E. W. Baxter, A. B. Reitz, J. Org. Chem. 59, 3175 (1994); C. R. R. Matos et al., Synthesis 1999, 571.
In vitro efficacy vs HIV: A. Karpas et al., Proc. Natl. Acad. Sci. USA 85, 9229 (1988). Inhibition of glycolipid biosynthesis: F. M. Platt et al., J. Biol. Chem. 269, 8362 (1994).
Clinical evaluation in Gaucher’s disease: T. Cox et al., Lancet 355, 1481 (2000). Review of pharmacology and clinical development in Gaucher’s disease: P. L. McCormack, K. L. Goa, Drugs 63, 2427-2434 (2003).
Properties: White to off-white crystalline solid, mp 125-126°. [a]D25 -15.9° (c = 0.77 in water). Highly sol in water (>1000 mg/ml).
Melting point: mp 125-126°
Optical Rotation: [a]D25 -15.9° (c = 0.77 in water)
Therap-Cat: In treatment of inherited glycosphingolipid lysosomal storage disorders.
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WORLD DRUG TRACKER
Capecitabine– treatment of metastatic breast and colorectal cancers.
Capecitabine, pentyl [1-(3,4-dihydroxy-5-methyltetrahydrofuran-2-yl)-5-fluoro-2-oxo-1H-pyrimidin-4-yl]carbamate
Capecitabine (Xeloda, Roche) is an orally-administered chemotherapeutic agent used in the treatment of metastatic breast and colorectal cancers. Capecitabine is a prodrug, that is enzymatically converted to 5-fluorouracil in the tumor, where it inhibits DNA synthesis and slows growth of tumor tissue.The activation of capecitabine follows a pathway with three enzymatic steps and two intermediary metabolites, 5′-deoxy-5-fluorocytidine (5′-DFCR) and 5′-deoxy-5-fluorouridine (5′-DFUR), to form 5-fluorouracil
Capecitabine is a chemotherapy drug that is administered as a treatment for a variety of cancer types, including bowel cancer, stomach cancer, breast cancer and oesophageal cancer. It acts as a prodrug, undergoing a three-step enzymic conversion into 5-fluorouracil in the tumour, where it inhibits DNA synthesis and thus slows growth of tumour tissue. Capecitabine can be synthesized from the readily available starting materials D-ribofuranose and cytosine [1].
When capecitabine is used for long-term treatment of recurrent cancers, one of the side-effects can be the onset of hand-foot syndrome, which eventually can lead to total eradication of the patients fingerprints [2]. This has recently proved rather inconvenient for one unsuspecting patient. A recent report [3] describes an instance where a patient on capecitabine for over three years went to the USA to visit relatives in December 2008. He was detained for 4 hours as his fingerprints could not be detected by immigration officials and was only allowed to enter after the officers were entirely satisfied that he posed no threat to security. As a result, all patients taking capecitabine long-term are being advised to travel with a letter from an oncologist stating condition and treatment being received to account for their lack of fingerprints.
As a final aside, recent reports suggest that the actual purpose of fingerprints is to enhance sensitivity rather than friction.
References
- Moon, B.S., Shim, A.Y., Lee, K.C., Lee, H.J., Lee, B.S., An, G.I., Yang, S. D., Chi, D.Y., Choi, C.W., Lim, S.M. and Chun, K.S. (2005) Synthesis of F-18 labeled capecitabine using [18F]F2 gas as a tumor imaging agent. Bull. Korean Chem. Soc. 26, 1865–1868.
- Chua, D., Wei, W.I., Sham, J.S.T. and Au, G.K.H. (2008) Capecitabine monotherapy for recurrent and metastatic nasopharyngeal cancer.Jpn. J. Clin. Oncol. 38, 244–249.
- Wong, M., Choo, S.-P. and Tan, E.-H. (2009) Travel warning with capecitabine. Annals of Oncology Advance Access May 26th 2009/doi:10.1093/annonc/mdp278.
http://promontory-science-education.webnode.com/animations/#.UbkbNtiNCS0
is link to below animation
Vitaros Approved in 10 Countries
Vitaros, alprostadil
7-[(1R,3R)-3-hydroxy-2-[(1E,3S)-3-hydroxyoct-1-en-1-yl]-5-oxocyclopentyl]heptanoic acid
Apricus Biosciences Inc. said that its impotence drug Vitaros has been approved in 10 European countries. The company said Vitaros is now approved in the Netherlands, Germany, France, Italy, and the U.K., among other countries, for the treatment of erectile dysfunction.
The active ingredient in Vitaros, alprostadil, is an ingredient in other approved impotence treatments and Apricus is also studying it as a treatment for female sexual arousal disorder.
Prostaglandin E1 (PGE1), known pharmaceutically as alprostadil,[1] is a prostaglandin. It is a drug used in the treatment of erectile dysfunction[2] and has vasodilatory properties.
Patent ductus arteriosus
Alprostadil is also used in maintaining a patent ductus arteriosus in newborns. This is primarily useful when there is threat of premature closure of the ductus arteriosus in an infant with ductal-dependent congenital heart disease, including cyanotic lesions (e.g., pulmonary atresia/stenosis, tricuspid atresia/stenosis, transposition of the great arteries) and acyanotic lesions (e.g., coarctation of the aorta, hypoplastic left heart syndrome, critical aortic stenosis, interrupted aortic arch).
Sexual dysfunction
Alprostadil is sold in the United States as urethral suppositories and in injectable form. The suppositories are sold under the brand name MUSE.[3] The injectable forms are Edex[4] and Caverject.[5] Muse delivers alprostadil as a penile suppository, inserted into the urethra, at least ten minutes before the erection will be needed. Caverject and Edex are similarly fast-acting, but instead are injected by syringe directly into the corpus cavernosum of the penis.
Apricus Biosciences is developing proprietary drugs; Vitaros for men with erectile dysfunction, Femprox for female sexual arousal disorder and RayVa for Raynaud’s phenomenon. Two Phase III studies have been completed for Vitaros, and approval has been granted in Canada. Apricus Biosciences is seeking regulatory approval in Europe, South America, and other territories. Apricus Biosciences sold the rights for Vitaros in the US to Warner Chilcott.[6]
Alprostadil is also available as a generic. The major cost is that it must be mixed by a compounding pharmacy and supplies of alprostadil may be difficult to obtain. There are different formulations, including Bimix and Trimix, which may include papaverine and/or phentolamine. A typical mix might be 30 mg of papaverine, 2 mg of phentolamine, and 20 mcg alprostadil. As a generic, it is much less expensive than the pre-packaged injectables. It is premixed and must be kept refrigerated and the user must load a syringe with the quantity needed.
Critical limb ischemia
Alprostadil is also used for critical limb ischemia. It increases blood flow by peripheral vasodilation within 5 minutes and induces angiogenesis. It is most effective when the ankle pressure is at least 30 mmHg and at least one tibial artery is patent.
- Cawello W, Leonhardt A, Schweer H, Seyberth HW, Bonn R, Lomeli AL (September 1995). “Dose proportional pharmacokinetics of alprostadil (prostaglandin E1) in healthy volunteers following intravenous infusion”. British Journal of Clinical Pharmacology 40 (3): 273–6. PMC 1365109. PMID 8527291.
- Harding LM, Adeniyi A, Everson R, Barker S, Ralph DJ, Baranowski AP (December 2002). “Comparison of a needle-free high-pressure injection system with needle-tipped injection of intracavernosal alprostadil for erectile dysfunction”. International Journal of Impotence Research 14 (6): 498–501. doi:10.1038/sj.ijir.3900916. PMID 12494285.
- “Muse Suppository – Facts and Comparisons”. Drugs.com. Retrieved 4 January 2013.
- Edex – Facts and Comparisons Drugs.com
- Caverject – Facts and Comparisons Drugs.com
- Fain Hughes (2007-10-29). “NEXM: Dutton Sees Strong Speculative Buy and 12-Month Price Double”. Retrieved 2007-11-01.
Prostaglandin E1 (alprostadil, PGE1) erectile dysfunction drug, molecular model. PGE1 is a prostaglandin used in the treatment of erectile dysfunction.
Study Finds Substances from African Medicinal Plants Could Help Stop Tumour Growth
Sections of the root of the giant globe thistle.
photo: Victor Kuete, Institute of Pharmaceutical Sciences and Biochemistry
African medicinal plants contain chemicals that may be able to stop the spread of cancer cells. This is the conclusion of researchers following laboratory experiments conducted at Johannes Gutenberg University Mainz (JGU). The plant materials will now undergo further analysis in order to evaluate their therapeutic potential.
“The active substances present in African medicinal plants may be capable of killing off tumour cells that are resistant to more than one drug. They thus represent an excellent starting point for the development of new therapeutic treatments for cancers that do not respond to conventional chemotherapy regimens,” explained Professor Thomas Efferth of the Institute of Pharmaceutical Sciences and Biochemistry – Therapeutic Life Sciences at Mainz University. For the past four years, Efferth and biochemist Dr. Victor Keute of the University of Dschang in Cameroon have been studying the active substances in African plants such as the giant globe thistle, wild pepper, speargrass, and Ethiopian pepper.
Krill oil is being studied as a natural remedy for high cholesterol
Krill Oil
Krill are shrimp-like crustaceans that are approximately 1 to 6 centimeters long. They live is the ocean, where they feed mainly on phytoplankton. They’re near the bottom of the food chain and are eaten by whales, seals, penguins, squid and fish.
Commercial fishing of krill occurs primarily in the Southern Ocean and the northern Pacific Ocean along the coasts of Canada and Japan. Krill that are caught are used for aquaculture and aquarium feeds, sport fishing bait or they are eaten as food. In Japan, krill that’s caught for food is called okiami.
Krill oil, the oil that’s found naturally in krill, is extracted and sold as a nutritional supplement. It’s sold in some health food stores and online in capsule form.
Krill oil contains omega-3 fatty acids, which is the main reason it’s becoming popular as a nutritional supplement.
Another reason krill oil is becoming popular is because it contains an antioxidant called astaxanthin. The algae that krill eat produces the bright red pigment astaxanthin that gives krill and other crustaceans such as lobster and shrimp their reddish-pink color.
Antioxidants protect our body cells from damage from free radicals, unstable substances that are thought to contribute to certain chronic diseases. Unlike many other antioxidants, astaxanthin crosses the blood-brain barrier, where it could theoretically protect the eye, brain and central nervous system from free radical damage.
The recent popularity of krill oil supplements has raised concerns that it could threaten the population of its predators, including penguins, seals and whales. people use krill oil for the same reasons they use fish oil, flax oil or other omega-3 fatty acids. Unlike fish oil, krill oil doesn’t cause fishy burps or an aftertaste, a common side effect of fish oil. Also, krill oil contains higher amounts of astaxanthin than fish oil. Here are some specific conditions for which it’s used.
1) High Cholesterol
Krill oil is being studied as a natural remedy for high cholesterol. In one study, 120 people were given krill oil, fish oil or a placebo. Krill oil reduced LDL (commonly referred to as “bad”) cholesterol by 34% and increased HDL (“good”) cholesterol by 43.5% compared to the placebo. In comparison, fish oil reduced LDL cholesterol by 4.6% and increased HDL cholesterol by 4.2%. Krill also lowered triglycerides.
2) Premenstrual Syndrome
Preliminary research suggests krill oil may help reduce symptoms of premenstrual syndrome (PMS), however, more research is needed.
Arthritis
A study in the Journal of the American College of Nutrition examined krill oil (300 mg daily) compared to a placebo and found that krill oil was effective at reducing arthritis symptoms and inflammation.
People with allergies to seafood shouldn’t use krill oil. People with bleeding disorders shouldn’t use krill oil unless under the supervision of a qualified health professional.
Side effects of krill oil may include loose stools, diarrhea or indigestion.
people taking blood thinners (anticoagulant or anti-platelet medication), such as aspirin, warfarin (Coumadin), heparin, clopidogrel (Plavix), non-steroidal anti-inflammatory medications (NSAIDS) such as ibuprofen (Motrin, Advil), naproxen (Naprosyn, Aleve) should only use krill oil under a physician’s supervision.
Krill oil should also be used with caution by people taking herbs and supplements that are thought to increase the risk of bleeding, such as ginkgo biloba and garlic.
Sources
Bunea R, El Farrah K, Deutsch L.Evaluation of the effects of Neptune Krill Oil on the clinical course of hyperlipidemia. Altern Med Rev. (2004) 9.4: 420-428.
Deutsch L. Evaluation of the effect of Neptune Krill Oil on chronic inflammation and arthritic symptoms. J Am Coll Nutr. (2007) 26.1: 39-48.
MORE INFO
Krill oil is a nutrient from a tiny crustacean (similar to a shrimp) that lives in the icy waters around the Antarctic. It is a rich source of the omega-3 essential fatty acids eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA).
The main selling points for krill oil are that its omega-3s are packaged differently from fish oils, in the form of a phospholipid that is easier for the body to absorb. This better absorption rate – up to 60 per cent, according to some manufacturers – means less capsules need to be taken to achieve the desired health benefits.
It is also said to have the added bonus of containing another essential nutrient, choline, as well as an antioxidant, astaxanthin. Astaxanthin is found in sea algae and it’s what gives shrimp, lobster, salmon, krill and other sea-life that feed on algae their rosy color.
Krill oil supplements are also more expensive than fish oils because of the extensive processes undertaken to ensure quality and eco-sustainability. However, many argue that it is better value for money, as you have to take less capsules than if you were taking fish oil.
Rare Undersea Discovery Could Extend Your Life by 10, 20 or 30 Years
Scientists are claiming that they have now isolated unusual ingredients in a rare seaweed discovered by fishermen off the coast of Korea that offer incredible health benefits—including the ability to restore blood pressure to normal levels.
The first is Seanol, an extremely rare seaweed extract from Ecklonia Cava that’s proven to be 100 times more powerful than any land-based antioxidant. That’s because it stays working in your body for 12 hours, compared to land-based antioxidants that work for 30 minutes.
“Its secret is its make-up of special polyphenol antioxidants that are a whopping 40% lipid (fat) soluble,” Dr. Lee explains. “Unlike nearly all land-based antioxidants that are water soluble, Seanol’s protective compounds can get into things like the fatty tissues of your brain and penetrate all three layers of your cells, including the outside, the oil-based cell membranes, and your DNA.”
Indeed, Seanol is so powerful, it’s the only FDA-approved Ecklonia Cava marine-algae extract in existence.
The second ingredient is Calamarine, a deep-sea omega-3 discovery that delivers 85% more DHA omega-3s to your heart, brain, joints, and eyes. It’s known to combat everything from fatigue and poor memory, to vision problems, joint pain, mood swings and depression.
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Ecklonia cava is an edible marine brown alga species found in the ocean off Japan andKorea.
It is used as a herbal remedy in the form of an extract called Seanol, a polyphenolic extract. Another phlorotannin-rich natural agent, Ventol, is also extracted from E. cava.[1]
Phlorotannins, such as fucodiphlorethol G,[2] 7-phloro eckol, 6,6′-bieckol,[3] eckol, 8,8′-bieckol, 8,4″‘-dieckol and phlorofucofuroeckol A can be isolated from Ecklonia cava.[4]
Other components are common sterol derivatives (fucosterol, ergosterol and cholesterol).[3]
A brownish colored seaweed, Ecklonia Cava
- Kang, K.; Hwang, H. J.; Hong, D. H.; Park, Y.; Kim, S. H.; Lee, B. H.; Shin, H. C. (2004). “Antioxidant and antiinflammatory activities of ventol, a phlorotannin-rich natural agent derived from Ecklonia cava, and its effect on proteoglycan degradation in cartilage explant culture”. Research communications in molecular pathology and pharmacology. 115-116: 77–95. PMID 17564307.
- Isolation of a New Phlorotannin, Fucodiphlorethol G, from a Brown Alga Ecklonia cava. Young Min Ham, Jong Seok Baik, Jin Won Hyun and Nam Ho Lee, Bull. Korean Chem. Soc. 2007, Vol. 28, No. 9 1595
- Li, Y.; Qian, Z. J.; Ryu, B.; Lee, S. H.; Kim, M. M.; Kim, S. K. (2009). “Chemical components and its antioxidant properties in vitro: An edible marine brown alga, Ecklonia cava”. Bioorganic & Medicinal Chemistry 17 (5): 1963–1973.doi:10.1016/j.bmc.2009.01.031. PMID 19201199.
- Ahn, M. J.; Yoon, K. D.; Min, S. Y.; Lee, J. S.; Kim, J. H.; Kim, T. G.; Kim, S. H.; Kim, N. G. et al. (2004). “Inhibition of HIV-1 reverse transcriptase and protease by phlorotannins from the brown alga Ecklonia cava”. Biological & pharmaceutical bulletin 27 (4): 544–547.PMID 15056863.
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Calamarine is new super DHA
One of the myths associated with aging is that your body wears out and there is nothing we can do about it. As we get older, we just have to live with chronic disease and the only way to improve the quality of our health and life is to treat the symptoms.
Overwhelmingly, research suggests that this is simply not true. In fact, the American Journal of Clinical Nutrition and Circulation provide documented evidence that consumption of Omega-3 fatty acids from dietary sources and supplements cut the likelihood of an early death.DHA and EPA not only prevent heart disease and sudden death from a sudden heart attack, they lower the risk…
A positive genotoxicity result can throw the fate of a promising drug candidate—in which a firm has invested significant time and money—into doubt
A positive genotoxicity result can throw the fate of a promising drug candidate-in which a firm has invested significant time and money-into doubt. The statistical improbability and challenges of bringing a drug to market become paramount.
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BY WORLD DRUG TRACKER
Automating Lead Optimization
This diagram illustrates the methods used to determine solubility as a compound advances toward further clinical study, and the increasing reach of automation and informatics systems. Initially, screens are run in silico on a library after hits are determined through a high-throughput screen; then various kinetic solubility assays are used to determine the compound’s potency at various concentrations. Two rounds of kinetic solubility assays determine gross and broad solubility (mmol/L) and finite solubility (less than 20 µmol/L) before the compound is advanced into thermodynamic solubility assays. Figure modified from Petereit A, Saal C. What is the Solubility of My Compound? Assessing Solubility for Pharmaceutical Research and Development Compounds. Am Pharm Rev. 2011; 14
The drug discovery business is changing rapidly. More pharmaceutical companies are working with smaller biotech firms to create early-stage compounds, and thus need quicker and standardized solutions to early-stage development problems.
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WORLD DRUGTRACKER
Gilead Announces U.S. FDA Priority Review Designation for Sofosbuvir for the Treatment of Hepatitis C
Sofosbuvir
Isopropyl (2S)-2-[[[(2R,3R,4R,5R)-5-(2,4-dioxopyrimidin-1-yl)-4-fluoro-3-hydroxy-4-methyl-tetrahydrofuran-2-yl]methoxy-phenoxy-phosphoryl]amino]propanoate
http://www.ama-assn.org/resources/doc/usan/sofosbuvir.pdf –for cas no
Jun. 7, 2013– Gilead Sciences, Inc. today announced that the U.S. Food and Drug Administration (FDA) has granted priority review to the company’s New Drug Application (NDA) for sofosbuvir, a once-daily oral nucleotide analogue inhibitor for the treatment of chronic hepatitis C virus (HCV) infection. The FDA grants priority review status to drug candidates that may offer major advances in treatment over existing options. Gilead filed the NDA for sofosbuvir on April 8, 2013, and FDA has set a target review date under the Prescription Drug User Fee Act (PDUFA) of December 8, 2013.
The data submitted in this NDA support the use of sofosbuvir and ribavirin (RBV) as an all-oral therapy for patients with genotype 2 and 3 HCV infection, and for sofosbuvir in combination with RBV and pegylated interferon (peg-IFN) for treatment-naïve patients with genotype 1, 4, 5 and 6 HCV infection.
Sofosbuvir is an investigational product and its safety and efficacy have not yet been established.
About Gilead Sciences
Gilead Sciences is a biopharmaceutical company that discovers, develops and commercializes innovative therapeutics in areas of unmet medical need. The company’s mission is to advance the care of patients suffering from life-threatening diseases worldwide. Headquartered in Foster City, California, Gilead has operations in North America, Europe and Asia Pacific.
Sofosbuvir (formerly PSI-7977 or GS-7977) is an experimental drug candidate for the treatment of hepatitis C.[1] It was discovered at Pharmasset and then acquired for development by Gilead Sciences. It is currently in Phase III clinical trials.[2]
Sofosbuvir is a prodrug that is metabolized to the active antiviral agent 2′-deoxy-2′-α-fluoro-β-C-methyluridine-5′-monophosphate.[3]
Sofosbuvir is a nucleotide analogue inhibitor of the hepatitis C virus (HCV) polymerase.[4] The HCV polymerase or NS5B protein is a RNA-dependent RNA polymerase critical for the viral cycle.
Sofosbuvir is being studied in combination with pegylated interferon and ribavirin, with ribavirin alone, and with other direct-acting antiviral agents.[5] It has shown excellent clinical efficacy when used either with pegylated interferon/ribavirin or in interferon-free combinations. In particular, combinations of sofosbuvir with NS5A inhibitors, such as daclatasvir or GS-5885, have shown sustained virological response rates of up to 100% in people infected with HCV.[6]
Data from the ELECTRON trial showed that a dual interferon-free regimen of sofosbuvir plus ribavirin produced a 24-week post-treatment sustained virological response (SVR24) rate of 100% for previously untreated patients with HCV genotypes 2 or 3.[7][8]
Data presented at the 20th Conference on Retroviruses and Opportunistic Infections in March 2013 showed that a triple regimen of sofosbuvir, ledipasvir (formerly GS-5885), and ribavirin produced a 12-week post-treatment sustained virological response (SVR12) rate of 100% for both treatment-naive patients and prior non-responders with HCV genotype 1.[9]Gilead has developed a sofosbuvir + ledipasvir coformulation that is being tested with and without ribavirin.
- Sofia, M. J.; Bao, D.; Chang, W.; Du, J.; Nagarathnam, D.; Rachakonda, S.; Reddy, P. G.; Ross, B. S. et al. (2010). “Discovery of a β-d-2′-Deoxy-2′-α-fluoro-2′-β-C-methyluridine Nucleotide Prodrug (PSI-7977) for the Treatment of Hepatitis C Virus”. Journal of Medicinal Chemistry 53 (19): 7202–7218. doi:10.1021/jm100863x. PMID 20845908. edit
- “PSI-7977″. Gilead Sciences.
- Murakami, E.; Tolstykh, T.; Bao, H.; Niu, C.; Steuer, H. M. M.; Bao, D.; Chang, W.; Espiritu, C. et al. (2010). “Mechanism of Activation of PSI-7851 and Its Diastereoisomer PSI-7977″. Journal of Biological Chemistry 285 (45): 34337–34347.doi:10.1074/jbc.M110.161802. PMC 2966047. PMID 20801890. edit
- Alejandro Soza (November 11, 2012). “Sofosbuvir”. Hepaton.
- Tom Murphy (November 21, 2011). “Gilead Sciences to buy Pharmasset for $11 billion”. Bloomberg Businessweek.
- http://www.gilead.com/pr_1757156
- AASLD: PSI-7977 plus Ribavirin Can Cure Hepatitis C in 12 Weeks without Interferon. Highleyman, L. HIVandHepatitis.com. 8 November 2011.
- Nucleotide Polymerase Inhibitor Sofosbuvir plus Ribavirin for Hepatitis C. Gane, E et al. New England Journal of Medicine 368:3444. January 3, 2013.
- CROI 2013: Sofosbuvir + Ledipasvir + Ribavirin Combo for HCV Produces 100% Sustained Response. Highleyman, L. HIVandHepatitis.com. 4 March 2013.
Eating Broccoli Reduces Risk of Cardiovascular Disease, Promotes Heart Health
by Elizabeth Renter , MY SCIENCE ACADEMY
It’s not good enough to know that vegetables like broccoli are healthful; we need to know specifically what sort of benefits they deliver, how they deliver those benefits and how we can make the most of them.
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New Drug Approvals 